The berbine class of heterocyclic compounds is structurally related to the plant alkaloid berberine. Berbine compounds have been reported to have numerous therapeutic effects. For example, they have been found to have antibacterial, antifungal, antiparasitic, antipyretic, antihypertensive, antidepressant, antiemetic, tranquilizing, and analgesic activities. Because of the potential therapeutic value of berbine compounds and derivatives thereof, there is a need for new derivatives than may be more potent and/or efficacious. Moreover, there is a need for efficient synthesis processes for the preparation of pure preparations of specific enantiomers of these substituted berbines.